Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) lead. Part II: development of a potent and highly selective M1 PAM
Research output: Contribution to journal › Journal article › Research › peer-review
This Letter describes a chemical lead optimization campaign directed at VU0119498, a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) with the goal of developing a selective M(1) PAM. An iterative library synthesis approach delivered a potent (M(1) EC(50)=830 nM) and highly selective M(1) PAM (>30 microM vs M(2)-M(5)).
| Original language | English |
|---|---|
| Journal | Bioorganic & Medicinal Chemistry Letters |
| Volume | 20 |
| Issue number | 6 |
| Pages (from-to) | 1972-5 |
| Number of pages | 4 |
| ISSN | 0960-894X |
| DOIs | |
| Publication status | Published - 15 Mar 2010 |
| Externally published | Yes |
Bibliographical note
Copyright 2010 Elsevier Ltd. All rights reserved.
- Allosteric Regulation, Cholinergic Agents/chemistry, Drug Design, Receptors, Muscarinic/drug effects, Structure-Activity Relationship
Research areas
ID: 213626845